TDG-IN-1

TDG-IN-1 is an orally active, selective small molecule inhibitor of thymine DNA glycosylase (TDG) with a Ka of 1.46 nM. It disrupts TDG's DNA binding ability, induces downregulation of DHX9 expression, leads to double-stranded RNA accumulation, and activates the RIG-I/MDA5-MAVS pathway. Additionally, it acts as a tumor suppressor, innate immune activator, and immune stimulator. TDG-IN-1 inhibits the growth of p53-deficient tumor cells and xenografts, exhibiting a synthetic lethal effect with p53. This compound is useful for research in p53-deficient cancers.